# Selective Androgen Receptor Modulators in Women: What Do We Know, and What Is Still Missing

**Authors:** Veselin Vasilev, Katerina Georgieva, Maria Kraeva, Raina Ardasheva, Rumyana Etova, Nikolay Boyadjiev

PMC · DOI: 10.3390/life16020359 · Life · 2026-02-20

## TL;DR

This paper reviews what is known about selective androgen receptor modulators (SARMs) in women, highlighting their potential benefits and gaps in understanding.

## Contribution

The paper provides a comprehensive review of preclinical and clinical evidence on SARMs in females, emphasizing the need for further sex-specific research.

## Key findings

- SARMs may enhance sexual motivation and improve muscle and bone outcomes in female rodent models.
- Clinical studies show SARMs increase lean body mass in postmenopausal women with limited androgenic effects.
- AR-targeted SARMs show antitumor activity in certain breast cancer subtypes.

## Abstract

Androgens and androgen receptor (AR) signaling influence many aspects of female physiology, including reproduction, musculoskeletal health, metabolism, and neurological regulation, yet are less studied than in males. Selective androgen receptor modulators (SARMs) were developed to provide tissue-selective anabolic effects with reduced androgenic side effects, but their effects in women are not well defined. This narrative review summarizes preclinical and clinical evidence on SARM use in female rodents and women, focusing on AR biology, tissue selectivity, therapeutic potential, and safety. A literature search of PubMed, Scopus, and Google Scholar identified relevant experimental and clinical studies addressing sex-specific AR signaling and SARM effects in females. Preclinical data indicate that SARMs can enhance sexual motivation and improve muscle and bone outcomes in ovariectomized models, with compound-dependent effects on reproductive tissues. Clinical studies in postmenopausal women demonstrate increases in lean body mass with generally limited androgenic effects, although functional benefits are inconsistent and alterations in lipid profiles and liver enzymes have been reported. Evidence also supports antitumor activity of AR-targeted SARMs in selected breast cancer subtypes. Overall, while SARMs show therapeutic potential in women, long-term safety and efficacy remain insufficiently characterized, warranting further sex-specific clinical investigation.

## Linked entities

- **Proteins:** AR (androgen receptor)
- **Diseases:** breast cancer (MONDO:0004989)
- **Species:** Mus musculus (taxon 10090)

## Full-text entities

- **Genes:** SLC17A5 (solute carrier family 17 member 5) [NCBI Gene 26503] {aka AST, ISSD, NSD, SD, SIALIN, SIASD}, IL6 (interleukin 6) [NCBI Gene 3569] {aka BSF-2, BSF2, CDF, HGF, HSF, IFN-beta-2}, Cs (citrate synthase) [NCBI Gene 170587], RIEG2 (Rieger syndrome 2) [NCBI Gene 6012] {aka ARS, RGS2}, ESR1 (estrogen receptor 1) [NCBI Gene 2099] {aka ER, ESR, ESRA, ESTRR, Era, NR3A1}, EREG (epiregulin) [NCBI Gene 2069] {aka EPR, ER, Ep}, PGR (progesterone receptor) [NCBI Gene 5241] {aka NR3C3, PR}, MMP13 (matrix metallopeptidase 13) [NCBI Gene 4322] {aka CLG3, MANDP1, MDST, MMP-13}, AR (androgen receptor) [NCBI Gene 367] {aka AIS, AR8, DHTR, HPCX3, HUMARA, HYSP1}, INS (insulin) [NCBI Gene 3630] {aka IDDM, IDDM1, IDDM2, ILPR, IRDN, MODY10}, GPT (glutamic--pyruvic transaminase) [NCBI Gene 2875] {aka AAT1, ALT, ALT1, GPT1, SGPT}, ERBB2 (erb-b2 receptor tyrosine kinase 2) [NCBI Gene 2064] {aka CD340, HER-2, HER-2/neu, HER2, MLN 19, MLN-19}, REN (renin) [NCBI Gene 5972] {aka ADTKD4, HNFJ2, RTD}, Fdxr (ferredoxin reductase) [NCBI Gene 79122] {aka AR}, SHBG (sex hormone binding globulin) [NCBI Gene 6462] {aka ABP, SBP, TEBG}
- **Diseases:** back pain (MESH:D001416), polycystic ovary syndrome (MESH:D011085), deaths (MESH:D003643), seborrhea (MESH:D012628), anemia (MESH:D000740), osteoporosis (MESH:D010024), SARM (MESH:D013734), bone loss (MESH:D001847), toxicities (MESH:D064420), bone marrow suppression (MESH:D001855), infertility (MESH:D007246), hypoactive sexual desire (MESH:D020018), cardiovascular disease (MESH:D002318), liver injury (MESH:D017093), cholestatic and hepatocellular damage (MESH:D056486), muscle loss (MESH:D009135), androgen-deficient (MESH:D014770), adiposity (MESH:D018205), breast cancer (MESH:D001943), gynecological disorders (MESH:D005831), anemia of chronic disease (MESH:D002908), acne (MESH:D000152), voice deepening (MESH:D014832), fracture (MESH:D050723), metabolic disturbances (MESH:D024821), injury to (MESH:D014947), headache (MESH:D006261), sarcopenia (MESH:D055948), hirsutism (MESH:D006628), muscle wasting (MESH:D009133), inflammatory (MESH:D007249), sexual dysfunction (MESH:D012735), cancer (MESH:D009369), myocarditis (MESH:D009205), cachexia (MESH:D002100), COPD (MESH:D029424), stress urinary incontinence (MESH:D014550), jaundice (MESH:D007565), nausea (MESH:D009325)
- **Chemicals:** Andarine (-), GSK-2881078 (MESH:C000627232), LGD-2226 (MESH:C515129), LGD-3303 (MESH:C535233), DHEA (MESH:D003687), lipid (MESH:D008055), alendronate (MESH:D019386), testosterone propionate (MESH:D043343), steroid (MESH:D013256), S-27 (MESH:C072789), dihydrotestosterone (MESH:D013196), RAD140 (MESH:C000627876), triglycerides (MESH:D014280), S-101479 (MESH:C582954), S-40503 (MESH:C540747), estradiol (MESH:D004958), testosterone (MESH:D013739), GTx-007 (MESH:C492992), GTx-024 (MESH:C547106), MK-0773 (MESH:C550076), S-23 (MESH:C031333), cholesterol (MESH:D002784), progesterone (MESH:D011374)
- **Species:** Homo sapiens (human, species) [taxon 9606], Rattus norvegicus (brown rat, species) [taxon 10116], Mus musculus (house mouse, species) [taxon 10090]
- **Cell lines:** MDA-MB-231 — Homo sapiens (Human), Breast adenocarcinoma, Cancer cell line (CVCL_0062)

## Full text

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## References

59 references — full list in the complete paper: https://tomesphere.com/paper/PMC12942610/full.md

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Source: https://tomesphere.com/paper/PMC12942610